NOVEL C-2 SUBSTITUTED CARBAPENEM DERIVATIVES PART IV - SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 5 MEMBERED HETEROAROMATIC DERIVATIVES

The synthesis, antibacterial activity, and stability to human dehydrop eptidase-1 (DHP-1) of a novel series of yethyl]-2-heterocyclylcarbapen -2-em-3-carboxylates are described. Of the compounds investigated 1,5- disubstituted pyrazol-3-yl and 3-substituted isoxazol-5-yl derivatives have the best combination of antibacterial activity and stability to DHP-1. They are particularly active against community-acquired respira tory tract pathogens and have stabilities to DHP-1 superior to that of meropenem.